Ferrocene and its derivatives constitute versatile and interesting scaffolds for the global chemical enterprise due to its multiple applications that range from biomedical to materials science. Ferrocene has proven to be an excellent bioisostere that improves bioactivity, such as anticancer, antimalarial, antioxidant, antimicrobial, low cytotoxicity, and high lipophilicity. Ferrocenyl derivatives such as chalcones, stilbenes, aromatic ethyne, and cannabidiol analogues, are the leading compounds in our research for the syntheses and characterization as well as their potential applications. These derivatives have been synthesized employing synthetic methodologies such as Claisen-Schmidt, Sonogashira, Heck, and other well know reactions, with moderate to good yields and applying a greener approach when possible. Among these derivatives, our interest is mainly focused in ferrocenyl chalcones as a framework for further derivatization. Some of the explored modifications consist on the incorporation of different substituents in the aromatic rings, heterocyclic aromatic moieties, coumarin, adamantane, urea and thiourea hybrides, among others, into the ferrocenyl chalcone core. Another modification explored is the formation of ammonium or pyridinium salts to increase water solubility. Studied ferrocenyl derivatives exhibit remarkable stability, physical, and electrochemical properties. These factors have led the approaches for them to be precursors of biologically active compounds (cancer, bacteria, malaria, and neurobiological diseases). Moreover, other potential applications include molecular materials, perovskite solar cells, and polymers.